Table of Contents

Introduction 170

Solubility 171

Solubility Methodology 171

Applications of Solubility in Lead Optimization 172

Strategies on Improving Solubility 174

Structural Modifications to Increase Solubility 174

Salt Form 176

Prodrug Approaches 176

Structure-Solubility Relationship 176

Introduction of Basic Nitrogen 176

Reduction of Crystal Packing Energy 178

Permeability 179

Oral Absorption 179

Transport Mechanisms for Oral Absorption 179

Permeability Methodology 179

Structure-Permeability Relationship 181

Blood-Brain Barrier 182

Blood Brain Barrier and Transport Mechanisms 182

Methodology for BBB Penetration 184

Structure-BBB Penetration Relationship 185

Cell-based Assays 187

Conclusions 189

Acknowledgements 190

References 190

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